Comparative Pharmacology
Head-to-head clinical analysis: BRETYLOL versus DOFETILIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BRETYLOL versus DOFETILIDE.
BRETYLOL vs DOFETILIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bretylium tosylate is an adrenergic neuron blocking agent that inhibits norepinephrine release and enhances its reuptake, resulting in postganglionic sympathetic blockade. It also has direct antiarrhythmic effects by increasing the ventricular fibrillation threshold.
Selectively blocks the rapid component of the delayed rectifier potassium current (Ikr) in cardiac myocytes, prolonging repolarization and the effective refractory period.
Intravenous: 5-10 mg/kg over 10 minutes, then 5-10 mg/kg every 6-8 hours as needed for arrhythmias. Intramuscular: 5-10 mg/kg, may repeat every 6-8 hours.
250-500 mcg orally twice daily, based on creatinine clearance and QTc response.
None Documented
None Documented
Clinical Note
moderateDofetilide + Levofloxacin
"Dofetilide may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderateDofetilide + Norfloxacin
"Dofetilide may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderateDofetilide + Gemifloxacin
"Dofetilide may increase the QTc-prolonging activities of Gemifloxacin."
Clinical Note
moderateDofetilide + Torasemide
"Dofetilide may increase the QTc-prolonging activities of Torasemide."
Terminal elimination half-life is 7-11 hours in normal renal function; prolonged in renal impairment (up to 30 hours)
Terminal elimination half-life: 10 hours (range 7–13 hours) in patients with normal renal function; prolonged in renal impairment, up to 20 hours in moderate impairment and >30 hours in severe impairment.
Primarily renal excretion of unchanged drug (80-90%); minor biliary/fecal elimination (10-20%)
Renal: 80% unchanged; biliary/fecal: 20% as metabolites and unchanged drug.
Category C
Category C
Antiarrhythmic (Class III)
Antiarrhythmic (Class III)